CN103261201B - 作为trpa1拮抗剂的2-氨基-4-芳基噻唑化合物 - Google Patents
作为trpa1拮抗剂的2-氨基-4-芳基噻唑化合物 Download PDFInfo
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- CN103261201B CN103261201B CN201180059690.2A CN201180059690A CN103261201B CN 103261201 B CN103261201 B CN 103261201B CN 201180059690 A CN201180059690 A CN 201180059690A CN 103261201 B CN103261201 B CN 103261201B
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- China
- Prior art keywords
- dioxo
- thiazol
- pyrimidin
- phenyl
- trifluoromethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- -1 [4- [2, 4-difluoro-3- (trifluoromethyl) phenyl ] -2- { [ (1, 3-dimethyl-2, 4-dioxo-1, 2,3, 4-tetrahydrothieno [2,3-d ] pyrimidin-5-yl) acetyl ] imino } -1, 3-thiazol-3 (2H) -yl ] methylphosphonic acid Chemical compound 0.000 claims description 172
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- C07D491/04—Ortho-condensed systems
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- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
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IN3451MU2010 | 2010-12-20 | ||
IN3451/MUM/2010 | 2010-12-20 | ||
US201061428327P | 2010-12-30 | 2010-12-30 | |
US61/428,327 | 2010-12-30 | ||
IN748/MUM/2011 | 2011-03-16 | ||
IN748MU2011 | 2011-03-16 | ||
US201161466535P | 2011-03-23 | 2011-03-23 | |
US61/466,535 | 2011-03-23 | ||
IN1569/MUM/2011 | 2011-05-25 | ||
IN1569MU2011 | 2011-05-25 | ||
US201161495002P | 2011-06-09 | 2011-06-09 | |
US61/495,002 | 2011-06-09 | ||
IN2741MU2011 | 2011-09-28 | ||
IN2741/MUM/2011 | 2011-09-28 | ||
US201161552076P | 2011-10-27 | 2011-10-27 | |
US61/552,076 | 2011-10-27 | ||
PCT/IB2011/003224 WO2012085662A1 (en) | 2010-12-20 | 2011-12-15 | 2-amino-4-arylthiazole compounds as trpa1 antagonists |
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CN103261201A CN103261201A (zh) | 2013-08-21 |
CN103261201B true CN103261201B (zh) | 2015-04-22 |
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EP (1) | EP2655377B1 (ru) |
JP (1) | JP5694560B2 (ru) |
KR (1) | KR101591153B1 (ru) |
CN (1) | CN103261201B (ru) |
AP (1) | AP3391A (ru) |
AR (1) | AR084294A1 (ru) |
AU (1) | AU2011346763B2 (ru) |
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CA (1) | CA2820448A1 (ru) |
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MY (1) | MY159059A (ru) |
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TW (1) | TWI515199B (ru) |
UA (1) | UA109916C2 (ru) |
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CA2742954C (en) | 2008-11-07 | 2018-07-10 | Massachusetts Institute Of Technology | Aminoalcohol lipidoids and uses thereof |
CA2820448A1 (en) | 2010-12-20 | 2012-06-28 | Glenmark Pharmaceuticals, S.A. | 2-amino-4-arylthiazole compounds as trpa1 antagonists |
RU2014108885A (ru) | 2011-08-09 | 2015-09-20 | Хайдра Байосайенсиз, Инк. | Ингибирование транзиторного рецепторного потенциала ионного канала trpa1 |
CA3119789A1 (en) | 2011-10-27 | 2013-05-02 | Massachusetts Institute Of Technology | Amino acid derivatives functionalized on the n-terminal capable of forming drug encapsulating microspheres |
WO2013108857A1 (ja) | 2012-01-17 | 2013-07-25 | 味の素株式会社 | 複素環アミド誘導体及びそれを含有する医薬 |
CN104350058A (zh) | 2012-06-08 | 2015-02-11 | 格兰马克药品股份有限公司 | 2-氨基-4-芳基噻唑化合物的酰胺及其盐 |
MY187910A (en) | 2012-10-01 | 2021-10-28 | Orion Corp | N-prop-2-ynyl carboxamide derivatives and their use as trpa1 antagonists |
US9394308B2 (en) | 2013-01-18 | 2016-07-19 | Merck Sharp & Dohme Corp. | Inhibiting the transient receptor potential A1 ion channel |
GB201309333D0 (en) | 2013-05-23 | 2013-07-10 | Agency Science Tech & Res | Purine diones as WNT pathway modulators |
US9198898B2 (en) | 2013-06-24 | 2015-12-01 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
US8906951B1 (en) | 2013-06-24 | 2014-12-09 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
EP3057583A2 (en) | 2013-10-15 | 2016-08-24 | Glenmark Pharmaceuticals S.A. | Pharmaceutical composition comprising a trpa1 antagonist and an analgesic agent |
JP2017507182A (ja) * | 2014-02-24 | 2017-03-16 | ザ・ジョンズ・ホプキンス・ユニバーシティ | Tmem100ペプチド及びその変異体、並びに疾患又は状態の処置又は予防におけるそれらの使用 |
FI3310764T3 (fi) | 2015-06-19 | 2023-07-18 | Massachusetts Inst Technology | Alkenyylillä substituoidut 2,5-piperatsiinidionit ja niiden käyttö koostumuksissa agenssin kuljettamiseksi subjektille tai soluun |
FR3037956B1 (fr) * | 2015-06-23 | 2017-08-04 | Servier Lab | Nouveaux derives d'acide amine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
WO2017060488A1 (en) | 2015-10-09 | 2017-04-13 | Almirall, S.A. | New trpa1 antagonists |
WO2017064068A1 (en) | 2015-10-14 | 2017-04-20 | Almirall, S.A. | New trpa1 antagonists |
CN108727400B (zh) * | 2017-05-24 | 2021-07-09 | 四川晶华生物科技有限公司 | 一种治疗肿瘤的化合物 |
US10710994B2 (en) | 2018-03-19 | 2020-07-14 | Genentech, Inc. | Oxadiazole transient receptor potential channel inhibitors |
BR112021007692A2 (pt) * | 2018-10-23 | 2021-08-10 | George Edward Hoag | composição e método para tratar os pulmões |
EP4045144A1 (en) * | 2019-10-15 | 2022-08-24 | Boehringer Ingelheim International Gmbh | Thienopyrimidones as trpa1 inhibitors |
CN114929712B (zh) * | 2019-10-15 | 2024-07-23 | 勃林格殷格翰国际有限公司 | 作为trpa1抑制剂的噻吩并嘧啶酮 |
IL297555A (en) * | 2020-04-22 | 2022-12-01 | George Edward Hoag | A method of treating a viral or bacterial infection using inhalation therapy |
CN111437275B (zh) * | 2020-05-14 | 2021-03-19 | 黑龙江中医药大学 | 一种用于外科手术后抗炎和镇痛的药物及其应用 |
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WO2009144548A1 (en) * | 2008-05-28 | 2009-12-03 | Glenmark Pharmaceuticals S.A. | Imidazo [2,1-b] purine derivatives as trpa1 modulators |
WO2010109328A1 (en) * | 2009-03-23 | 2010-09-30 | Glenmark Pharmaceuticals, S.A. | Isothiazolo-pyrimidinedione derivatives as trpa1 modulators |
WO2010125469A1 (en) * | 2009-04-29 | 2010-11-04 | Glenmark Pharmaceuticals, S.A. | Pyrimidinedione-fused heterocyclic compounds as trpa1 modulators |
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JP2006523237A (ja) | 2003-04-03 | 2006-10-12 | セマフォア ファーマシューティカルズ, インコーポレイテッド | Pi−3キナーゼインヒビタープロドラッグ |
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WO2010004390A1 (en) | 2008-06-17 | 2010-01-14 | Glenmark Pharmaceuticals, S.A. | Quinazoline dione derivatives as trpa1 modulators |
WO2009158719A2 (en) | 2008-06-27 | 2009-12-30 | Hydra Biosciences, Inc. | Methods and compositions for treating disorders |
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SG184767A1 (en) | 2009-03-23 | 2012-10-30 | Glenmark Pharmaceuticals Sa | Furopyrimidinedione derivatives as trpa1 modulators |
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WO2009144548A1 (en) * | 2008-05-28 | 2009-12-03 | Glenmark Pharmaceuticals S.A. | Imidazo [2,1-b] purine derivatives as trpa1 modulators |
WO2010109328A1 (en) * | 2009-03-23 | 2010-09-30 | Glenmark Pharmaceuticals, S.A. | Isothiazolo-pyrimidinedione derivatives as trpa1 modulators |
WO2010125469A1 (en) * | 2009-04-29 | 2010-11-04 | Glenmark Pharmaceuticals, S.A. | Pyrimidinedione-fused heterocyclic compounds as trpa1 modulators |
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